Yield:690998-90-4 99%

Reaction Conditions:

with hydrogen;palladium 10% on activated carbon in ethanol; under 2585.81 Torr; for 24 h;

Steps:

H.C Step C-Preparation of 4-(N-TERT-BUTOXYCARBON L-N-ISOPROPYLAMINOPIPERIDINE

A solution of L-BENZYL-4- (N-TERT-BUTOXYCARBONYL-N-ISOPROPYLAMINO) piperidine (79.0 g, 0.24 mol) in ethanol (140 mL) was flushed with nitrogen for 15 minutes. This solution was then added to a 2 L Parr flask containing a mixture of 10% palladium on carbon (15.8 G ; ca. 50 % wt. water) in ethanol (LOOML), which solution had been flushed with nitrogen for 15 minutes. This reaction mixture was placed on a Parr Shaker under hydrogen at 50 psi for 24 hours. The reaction mixture was filtered through a pad of Celite and the Celite washed with ethanol. The filtrate was then concentrated in vacuo to afford 57.0 g of the title intermediate as a white solid (>99% yield).

References:

WO2004/41806,2004,A2 Location in patent:Page 67